A review of the literature concerning the synthesis and pharmacology of benzophenanthridine and protoberberine alkaloids is presented with emphasis on the recently discovered antileukemic activity of certain members of these classes. A new synthetic approach is proposed in which the condensation of certain Schiff bases with homophthalic anhydrides is the convergent step in the production of key intermediates which can then be transformed into a variety of naturally occurring alkaloids within these classes by known methods. The advantages of a late-stage convergence followed by divergence to multiple targets in a synthetic pathway are discussed. This strategy should also allow the preparation of a wide variety of structurally related molecules which will allow a study of pharmacological structure-activity relationships. Compounds prepared in this study will be tested for antileukemic activity in mammalian cell culture and also in in vivo tumor systems.